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Akynzeo (FOSNETUPITANT)
Akynzeo works by blocking the action of substance-P, a natural substance in the body that triggers nausea and vomiting.
At a glance
| Generic name | FOSNETUPITANT |
|---|---|
| Sponsor | Helsinn Hlthcare |
| Drug class | Serotonin-3 Receptor Antagonist [EPC] |
| Target | Substance-P receptor |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
| First approval | 2018 |
Mechanism of action
Netupitant is selective antagonist of human substance P/neurokinin (NK-1) receptors.Palonosetron is 5-HT3 receptor antagonist with strong binding affinity for this receptor and little or no affinity for other receptors. Cancer chemotherapy may be associated with high incidence of nausea and vomiting, particularly when certain agents, such as cisplatin, are used. 5-HT3 receptors are located on the nerve terminals of the vagus in the periphery and centrally in the chemoreceptor trigger zone of the area postrema. Chemotherapeutic agents produce nausea and vomiting by stimulating the release of serotonin from the enterochromaffin cells of the small intestine. Serotonin then activates 5-HT3 receptors located on vagal afferents to initiate the vomiting reflex. The development of acute emesis is known to depend on serotonin and its 5-HT3 receptors have been demonstrated to selectively stimulate the emetic response.Delayed emesis has been largely associated with the a
Approved indications
- Chemotherapy-induced nausea and vomiting
Common side effects
- Headache
- Asthenia
- Fatigue
- Dyspepsia
- Erythema
- Constipation
- Anthracyclines and Cyclophosphamide Based Chemotherapy
Key clinical trials
- An Efficacy and Safety Study of Intravenous Palonosetron Administered as an Infusion and as a Bolus for the Prevention of Nausea and Vomiting (PHASE3)
- An Efficacy and Safety Study of Oral Netupitant and Palonosetron for the Prevention of Nausea and Vomiting (PHASE3)
- A Safety Study of Oral Netupitant and Palonosetron for the Prevention of Nausea and Vomiting (PHASE3)
- An Efficacy and Safety Study of Oral and Intravenous Palonosetron for the Prevention of Nausea and Vomiting (PHASE3)
- Study With IV NEPA (Fosnetupitant/Palonosetron) for the Prevention of Chemotherapy-induced Nausea and Vomiting in Paediatric Cancer Patients Undergoing Highly Emetogenic Chemotherapy (HEC) (PHASE2)
- A Clinical Trial to Assess Safety and Pharmacokinetics of Fosnetupitant 235 mg and Metabolites in Healthy Volunteers (PHASE1)
- A Study to Assess the Safety and the Efficacy of IV Fosnetupitant/Palonosetron (260 mg/0.25 mg) Combination Compared to Oral Netupitant/Palonosetron (300 mg/0.5 mg) Combination for the Prevention of CINV in AC Chemotherapy in Women With Breast Cancer (PHASE3)
Patents
| Patent | Expiry | Type |
|---|---|---|
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Akynzeo CI brief — competitive landscape report
- Akynzeo updates RSS · CI watch RSS
- Helsinn Hlthcare portfolio CI